Part IV: Design, synthesis and antitumor activity of fluoroquinolone C-3 heterocycles: bis-oxadiazole methylsulfide derivatives derived from ciprofloxacin / 药学学报
Acta Pharmaceutica Sinica
; (12): 1017-1022, 2012.
Article
em En
| WPRIM
| ID: wpr-276206
Biblioteca responsável:
WPRO
ABSTRACT
To explore an efficient strategy for further development of anticancer fluoroquinolone candidates derived from ciprofloxacin, a heterocyclic ring as the bioisosteric replacement of C3 carboxyl group led to a key intermediate, oxadiazole thiol (5), which was further modified to the bis-oxadiazole methylsulfides (7a-7h) and the corresponding dimethylpiperazinium iodides (8a-8h), respectively. Structures were characterized by elemental analysis and spectra data, and their anticancer activities in vitro against CHO, HL60 and L1210 cancer cells were also evaluated by MTT assay. The preliminary results show that piperazinium compounds (8) possess more potent activity than that of corresponding free bases (7).
Texto completo:
1
Índice:
WPRIM
Assunto principal:
Oxidiazóis
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Farmacologia
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Piperazinas
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Desenho de Fármacos
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Estrutura Molecular
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Leucemia L1210
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Ciprofloxacina
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Química
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Cricetulus
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Células CHO
Limite:
Animals
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Humans
Idioma:
En
Revista:
Acta Pharmaceutica Sinica
Ano de publicação:
2012
Tipo de documento:
Article